A compound represented by the formula
wherein R
1
, R
2
, R
3
and R
6
are the same or different and each is a hydrogen atom or a substituent; one of R
4
and R
5
is a hydrogen atom and the other is a group represented by the formula: —C(═X)—R
7
wherein X is N—O—R
8
or N—NH—R
9
wherein R
8
and R
9
are the same or different and each is a hydrogen atom or a group bonded via a carbon atom; and R
7
is a hydrogen atom or a substituent, and the like and a salt thereof have a superior IκB kinase inhibitory activity, and useful as pharmaceutical agents such as agents for preventing or treating diabetes and the like.
The invention provides a compound of Formula (I)
or a pharmaceutically acceptable salt of the compound, wherein R
1
, R
2
, R
3
and R
4
are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
Conjugates of CC-1065 analogs and bifunctional linkers
申请人:SYNTARGA BV
公开号:US11052155B2
公开(公告)日:2021-07-06
This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
本发明涉及 DNA 烷基化剂 CC-1065 的新型类似物及其共轭物。此外,本发明还涉及制备上述制剂和共轭物的中间体。这些共轭物的设计目的是在一个或多个活化步骤之后和/或以共轭物控制的速率和时间跨度释放它们的(多重)有效载荷,以便选择性地递送和/或可控地释放一种或多种所述 DNA 烷化剂。这些制剂、共轭物和中间体可用于治疗以不希望的(细胞)增殖为特征的疾病。例如,本发明的制剂和共轭物可用于治疗肿瘤。
6-AZAINDOLE COMPOUND
申请人:Takeda Pharmaceutical Company Limited
公开号:EP1732566A2
公开(公告)日:2006-12-20
Novel Conjugates of CC-1065 Analogs and Bifunctional Linkers
申请人:SYNTARGA BV
公开号:US20170274090A1
公开(公告)日:2017-09-28
This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.